| Bioactivity | PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation[1][2]. |
| CAS | 1609465-78-2 |
| Formula | C22H21ClN6O2 |
| Molar Mass | 436.89 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Benson M J, et al. Modeling the clinical phenotype of BTK inhibition in the mature murine immune system[J]. The Journal of Immunology, 2014, 193(1): 185-197. [2]. Schnute M E, et al. Aminopyrazole carboxamide bruton’s tyrosine kinase inhibitors. irreversible to reversible covalent reactive group tuning[J]. ACS Medicinal Chemistry Letters, 2018, 10(1): 80-85. |
PF-303
CAS: 1609465-78-2 F: C22H21ClN6O2 W: 436.89
PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 form
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